A1,
A2,
B,
C1,
C2,
D,
E,
F,
G-H,
I-K,
L,
M,
N,
O,
P1,
P2,
Q-R,
S,
T,
U-V,
W-Z
Rescula Pharmacology, Pharmacokinetics, Studies, Metabolism - Unoprostone isopropyl
Rescula Pharmacology, Pharmacokinetics, Studies, Metabolism - Unoprostone isopropyl
CLINICAL PHARMACOLOGY
Mechanism of Action
When instilled in the eye, RESCULAâ
is believed to reduce elevated intraocular pressure (IOP), by increasing the
outflow of aqueous humor, but the exact mechanism is unknown at this time.
Pharmacokinetics / Pharmacodynamics:
Absorption: After application to the eye, unoprostone isopropyl
is absorbed through the cornea and conjunctival epithelium where it is hydrolyzed
by esterases to unoprostone free acid.
A study conducted with 18 healthy volunteers dosed bilaterally
with unoprostone isopropyl ophthalmic solution twice daily for 14 days demonstrated
little systemic absorption of unoprostone isopropyl. The systemic exposure of
its metabolite unoprostone free acid was minimal following the ocular administration.
Mean peak unoprostone free acid concentration was less than 1.5 ng/mL. Little
or no accumulation of unoprostone free acid was observed.
Elimination: Elimination of unoprostone free acid from human
plasma is rapid, with a half-life of 14 minutes. Plasma levels of unoprostone
free acid dropped below the lower limit of quantitation (< 0.25 ng/mL) 1
hour following ocular instillation. The metabolites are excreted predominately
in urine.
Clinical Studies
Clinical studies showed that in patients with mean baseline
IOP of 23 mm Hg, RESCULAâ lowers
intraocular pressure by approximately 3-4 mm Hg throughout the day. RESCULAâ
appears to lower intraocular pressure without affecting cardiovascular or pulmonary
function.
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